Department of Pharmacy, Kaiser Permanente of Ohio, Parma, USA.
Ann Pharmacother. 2012 Jul-Aug;46(7-8):1033-46. doi: 10.1345/aph.1M721. Epub 2012 Jul 24.
To provide a clinical overview of the antipsychotic lurasidone.
Articles were identified by searching the MEDLINE, PubMed, Cochrane Library, and EBSCO databases (through February 2012) using the key word lurasidone. The manufacturer provided information on unpublished Phase 2 and 3 trials. The Clinicaltrials.gov database was reviewed for the status of ongoing and upcoming trials.
All clinical trials lasting longer than 3 weeks and published in the English language were selected for review. Additional documentation, including the product dossier, package insert, and poster presentations supplied by the publisher, was also evaluated.
Lurasidone hydrochloride is an atypical antipsychotic that is approved for the treatment of schizophrenia. It is under investigation for treatment of bipolar I disorder. It should be administered with food, is pregnancy category B, is contraindicated for coadministration with strong CYP3A4 inducers and inhibitors, and requires dose adjustments with certain medications and in renal and hepatic impairment. Like other atypical antipsychotics, lurasidone possesses dopamine D(2) and serotonin 5-HT(2A) antagonism but exhibits little affinity for histamine H(1), α(1)-adrenergic, or cholinergic M1 receptors. Additionally, it is a potent 5-HT(7) antagonist, which may impact depression and cognition. Phase 3 trial results revealed that 40-80 mg administered once daily resulted in statistically significant improvements in schizophrenia symptomatology compared with placebo. Lurasidone's rate of metabolic adverse events is low relative to other atypical antipsychotics; however, this is offset by dose-dependent increases in somnolence, akathisia, and parkinsonism.
Lurasidone has shown efficacy when compared to placebo in acute schizophrenia. Full characterization of the adverse effect profile and cognitive and affective benefits requires publication of trials with longer durations.
提供一种抗精神病药鲁拉西酮的临床概述。
通过使用关键词鲁拉西酮，在 MEDLINE、PubMed、Cochrane 图书馆和 EBSCO 数据库（截至 2012 年 2 月）中搜索文章，确定了文章。制造商提供了未发表的 2 期和 3 期试验的信息。检索 Clinicaltrials.gov 数据库以了解正在进行和即将进行的试验的状态。
选择持续时间超过 3 周并以英文发表的所有临床试验进行审查。还评估了其他文件，包括出版商提供的产品档案、包装说明书和海报介绍。
盐酸鲁拉西酮是一种新型抗精神病药，已获准用于治疗精神分裂症。它正在被研究用于治疗双相情感障碍 I 型。它应与食物一起服用，妊娠分类为 B，禁忌与强 CYP3A4 诱导剂和抑制剂合用，需要根据某些药物和肾功能及肝功能损害调整剂量。与其他新型抗精神病药一样，鲁拉西酮具有多巴胺 D2 和 5-HT2A 拮抗作用，但对组胺 H1、α1-肾上腺素能和毒蕈碱 M1 受体亲和力较低。此外，它还是一种有效的 5-HT7 拮抗剂，可能影响抑郁和认知。3 期试验结果表明，与安慰剂相比，每天一次服用 40-80mg 可显著改善精神分裂症症状。与其他新型抗精神病药相比，鲁拉西酮的代谢不良事件发生率较低；然而，这被剂量依赖性增加的镇静、静坐不能和帕金森症所抵消。
与安慰剂相比，鲁拉西酮在急性精神分裂症中显示出疗效。需要发表更长时间的试验，以全面描述不良反应谱和认知及情感获益。
